AZ 13824374

Pricing Availability   Qty
Description: Potent and selective ATAD2 bromodomain inhibitor
Chemical Name: (1R,2R,5S)-11-(8-((1-(2-Fluoro-2-methylpropyl)piperidin-4-yl)amino)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl)-2-isopropyl-2,3,5,6-tetrahydro-1,5-epiminobenzo[d]azocin-4(1H)-one
Purity: ≥98% (HPLC)
Literature (5)

Biological Activity for AZ 13824374

AZ 13824374 is a potent and selective inhibitor of ATPase family AAA domain-containing protein 2 (ATAD2) bromodomain (pIC50 values are 6.2 and 8.2 in NanoBRET assay and FRET assay, respectively). It is >100-fold selective over a range of epigenetic targets from ROMOscan panel (DiscoveRx Corp.). AZ 13824374 shows cellular target engagement (cellular inhibition pIC50 = 6.9) and antiproliferative activity in a range of breast cancer cell lines.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data for AZ 13824374

M. Wt 562.69
Formula C30H39FN8O2
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 162422438
Smiles CC(C)[C@H]1NC([C@@H]2CC3=C([C@H]1N2C(C4=NN5C(C)=NN=C5C(NC6CCN(CC6)CC(F)(C)C)=C4)=O)C=CC=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ 13824374

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 56.27 100
ethanol 56.27 100

Preparing Stock Solutions for AZ 13824374

The following data is based on the product molecular weight 562.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.78 mL 8.89 mL 17.77 mL
5 mM 0.36 mL 1.78 mL 3.55 mL
10 mM 0.18 mL 0.89 mL 1.78 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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References for AZ 13824374

References are publications that support the biological activity of the product.

Winter-Holt et al (2022) Discovery of a potent and selective ATAD2 bromodomain inhibitor with antiproliferative activity in breast cancer models. J.Med.Chem. 65 3306 PMID: 35133824

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Keywords: AZ 13824374, AZ 13824374 supplier, AZ13824374, potent, selective, inhibitors, inhibits, ATAD2, bromodomain, antiproliferative, AAA, domain-containing, protein, 2, Bromodomains, 7757, Tocris Bioscience

Citations for AZ 13824374

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Cancer Research Product Guide

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